US5306716AExpiredUtility

Methods of achieving antileukemia activity using 16-membered-macrolide-type compounds

Assignee: MERCK & CO INCPriority: Mar 20, 1992Filed: Mar 20, 1992Granted: Apr 26, 1994
Est. expiryMar 20, 2012(expired)· nominal 20-yr term from priority
A61K 31/70A61K 31/365A61P 35/02A61K 31/335
37
PatentIndex Score
6
Cited by
17
References
6
Claims

Abstract

Inhibition of renal cancer, melanoma, colon cancer, lung cancer and leukemia cells by administration of compounds from the bafilomycin and hygrolidin groups of compounds.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
       1. A method of treating leukemia cells in a mammal in need thereof, comprising the step of administering to said mammal a pharmacologically effective amount of a compound selected from the group consisting of a hygrolidin of the formula ##STR35## where R 10  is ##STR36## and R 11  is hydrogen, ##STR37## 
     
     
       2. The method as claimed in claim 1, wherein said compound administered to said mammal is ##STR38## 
     
     
       3. A method of treating leukemia cells in a mammal in need thereof, comprising the step of administering to said mammal a pharmacologically effective amount of bafilomycin of the formula   ______________________________________                                    
 ##STR39##                                                                
Compound                                                                  
        R.sup.1  R.sup.2                                                  
______________________________________                                    
(1)     H                                                                 
                  ##STR40##                                               
(4)     H                                                                 
                  ##STR41##                                               
(5)     H                                                                 
                  ##STR42##                                               
(6)     H                                                                 
                  ##STR43##                                               
(7)     H                                                                 
                  ##STR44##                                               
(8)                                                                       
         ##STR45##                                                        
                  ##STR46##                                               
(9)     H                                                                 
                  ##STR47##                                               
(10)                                                                      
         ##STR48##                                                        
                  ##STR49##                                               
(11)    H                                                                 
                  ##STR50##                                               
______________________________________                                    
     
     
     
       4. The method as claimed in claim 3, wherein said compound administered to said mammal is ##STR51## 
     
     
       5. A method of treating leukemia cells in a mammal in need thereof, comprising the step of administering to said mammal a pharmacologically effective amount of bafilomycin of the formula ##STR52## wherein:   ______________________________________                                    
Compound  R.sup.1    R.sup.3  R.sup.4                                     
______________________________________                                    
(12)      H          H                                                    
                               ##STR53##                                  
(14)                                                                      
           ##STR54##                                                      
                      ##STR55##                                           
                               ##STR56##                                  
______________________________________                                    
     
     
     
       6. A method of treating leukemia cells in a mammal in need thereof, comprising the step of administering to said mammal a pharmacologically effective amount of bafilomycin of the formula ##STR57## wherein:   ______________________________________                                    
Compound  R.sup.1       R.sup.5 R.sup.6                                   
______________________________________                                    
(15)      H             CH.sub.3                                          
                                CH.sub.3                                  
(16)                                                                      
           ##STR58##    CH.sub.3                                          
                                CH.sub.3                                  
(17)      H             H       OH                                        
                                or                                        
(18)      H             H       CH.sub.3.                                 
______________________________________

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